| DC75275 |
DDP-38003 2HCl |
DDP-38003 2HCl is an orally available inhibitor of histone lysine-specific demethylase 1A (LSD1). |
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| DC75276 |
Resminostat HCl |
Resminostat is an orally bioavailable inhibitor of histone deacetylase 1 (HDAC1), HDAC3, and HDAC6 (IC50s = 43-72 nM), |
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| DC75277 |
ICI-199441 HCl |
ICI-199441 HCl is a highly potent κ agonist. ICI 199441 was found to strongly inhibit the activity of cytochrome P450 2D6 (CYP2D6) (1: CYP2D6 IC50=26 nM). |
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| DC75278 |
Daunorubicin free base |
Daunorubicin exhibits cytotoxic activity through topoisomerase-mediated interaction with DNA, thereby inhibiting DNA replication and repair and RNA and protein synthesis. |
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| DC75279 |
Onvansertib free base |
Onvansertib, also know as NMS-P937, PCM-075 and NMS1286937, is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Onvansertib selectively inhibits PLK1, inducing selective G2/M cell-cycle arrest followed by apoptosis in a variety of tumor cells while causing reversible cell-cycle arrest at the G1 and G2 stages without apoptosis in normal cells. PLK1 inhibition may result in the inhibition of proliferation in PLK1-overexpressing tumor cells. PLK1 is a serine/threonine protein kinase crucial in the regulation of mitosis. |
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| DC75280 |
JQ1-Carboxylic acid |
JQ1-Carboxylic acid also known as JQ1 Acid, is an inhibitor of bromodomain and extra terminal domain (BET) family proteins. |
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| DC75281 |
WCK-4234 sodium |
WCK-4234 is a potent β-lactamase inhibitor. WCK-4234 inhibited class A, C and D β-lactamases with unprecedented k2/K values against OXA carbapenemases. WCK-4234 inhibited class A, C and D β-lactamases with unprecedented k2/K values against OXA carbapenemases. WCK-4234 formed highly stable acyl-complexes via mass spectrometry. WCK-4234 is a novel β-lactamase inhibitor that demonstate potent cross-class inhibition and clinical studies targeting MDR infections are warranted. |
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| DC75282 |
Levomilnacipran HCl |
Levomilnacipran (brand name Fetzima) is an antidepressant approved for the treatment of major depressive disorder in the United States. It was developed by Forest Laboratories and Pierre Fabre Group, and was approved by the Food and Drug Administration in July 2013. Levomilnacipran is the levo- enantiomer of milnacipran, and has similar effects and pharmacology, acting as a serotonin-norepinephrine reuptake inhibitor (SNRI). (Source: http://en.wikipedia.org/wiki/Levomilnacipran) |
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| DC75283 |
PNU112455A |
PNU112455A is an ATP site competetive inhibitor of CDK2 and CDK5. PNU112455A effectively upregulates the tumorous PD-L1 level, promotes the response to anti-PD-1 immunotherapy,and prolongs the survival time of mice bearing HCC tumors. |
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| DC75284 |
GSK2983559-AM |
GSK2983559-AM, also known as GSK2983559 active metabolite, is an active metabolite of GSK2983559, also known as RIPK2-IN-1, is a potent and selective inhibitor of receptor interacting protein-2 (RIP2) kinase. |
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| DC75285 |
TPT-172 HCl (R33) |
TPT-172, also known as R33 (described in Mecozzi et al' s paper), is a thiophene thiourea derivative with molecule weight 172 in free base form. There is no formal name yet, we temporally call this molecule as TPT-172. |Please also see similar products: TPT-197; TPT-260; TPT-172. |
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| DC75286 |
Tozasertib (VX-680) |
Tozasertib, also known as VX-680, MK0457 or VE465, is a synthetic, small-molecule Aurora kinase inhibitor with potential antitumor activity. Tozasertib binds to and inhibits Aurora kinases (AKs), thereby inducing apoptosis in tumor cells in which AKs are overexpressed. AKs, a family of serine-threonine kinases, are essential for mitotic progression, spindle formation, centrosome maturation, chromosomal segregation, and cytokinesis. |
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| DC75287 |
Topotecan HCl |
Topotecan is a topoisomerase inhibitor. It is a synthetic, water-soluble analog of the natural chemical compound camptothecin. In physiological environments, topotecan is in equilibrium with its inactive carboxylate form. Topotecan's active lactone form intercalates between DNA bases in the topoisomerase-I cleavage complex. The binding of topotecan in the cleavage complex prevents topoisomerase-I from religating the nicked DNA strand after relieving the strain. This intercalation therefore traps the topoisomerase-I in the cleavage complex bound to the DNA. When the replication-fork collides with the trapped topoisomerase-I, DNA damage occurs. This disruption prevents DNA replication and ultimately leads to cell death. |
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| DC75288 |
TIC-10 Isomer |
TIC10 isomer is an isomer and the "inactive version" of TIC10 (or ONC201). TIC-10 isomer was introduced to the research community since it was structurally wrong-assigned as the bioactive TIC-10 during early stage development of TIC-10 (now called ONC-201). TIC-10 isomer was found to be inactive, which did not reduce the viability of cancer cells. TIC-10 isomer may be used as a reference compound to compare with ONC-201. |
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| DC75289 |
THZ1 |
THZ1 is a selective CDK7 inhibitor that preferentially diminishes transcription in cancer cells. THZ1 has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7. Cancer cell-line profiling indicates that a subset of cancer cell lines, including human T-cell acute lymphoblastic leukaemia (T-ALL), have exceptional sensitivity to THZ1. Cyclin-dependent kinases (CDKs) are involved in temporal control of the cell cycle and transcription and play central roles in cancer development and metastasis. |
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| DC75290 |
Zotiraciclib free base |
Zotiraciclib, also known as TG02 and SB1317, is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. Zotiraciclib may be useful for the treatment of cancer that crosses the blood brain barrier and acts by depleting Myc through the inhibition of cyclin-dependent kinase 9 (CDK9). It is one of a number of CDK inhibitors under investigation; others targeting CDK9 for the treatment of acute myeloid leukemia include alvocidib and atuveciclib. Myc overexpression is a known factor in many cancers, with 80 percent of glioblastomas characterized by this property. |
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| DC75291 |
Tea Polyphenol (TP98) |
Tea polyphenol, also called green tea extract, are a mixture of chemical compounds, such as flavanoids and tannins, found naturally in tea. These chemical compounds are believed to be beneficial to human health, and they are the basis of many claims made about the health benefits of tea. Polyphenols are powerful antioxidants, which can reduce the risk of developing coronary artery disease and a number of other health problems. The compounds found in tea have also been linked with cancer reduction. |
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| DC75292 |
Tariquidar |
Tariquidar, also known as XR9576, is a P-glycoprotein (P-gp) inhibitor undergoing research as an adjuvant against multidrug resistance in cancer. Tariquidar non-competitively binds to the p-glycoprotein transporter, thereby inhibiting transmembrane transport of anticancer drugs. Inhibition of transmembrane transport may result in increased intracellular concentrations of an anticancer drug, thereby augmenting its cytotoxicity. |
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| DC75293 |
Talaporfin sodium |
Talaporfin sodium is a natural chlorophyll-based, and water soluble PDT photosensitizer consisting of chlorin e6, derived from chlorophyll, and L-aspartic acid with photosensitizing activity. After intratumoral activation by light emitting diodes, talaporfin sodium forms an extended high energy conformational state that generates singlet oxygen, which can kill target tissues with minimal side effects through vascular closure and apoptosis. Constant illumination can activate each molecule of talaporfin many times, resulting in a continuous supply of singlet oxygen molecules. Talaporfin kills all tumour cells in the targeted zone, rather than only the minority of cells undergoing rapid division, as in the case of chemotherapy. |
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| DC75294 |
Fasiglifam |
Fasiglifam, also known as TAK-875, is a potent, selective, and orally bioavailable GPR40 agonist, with a pharmacokinetic profile enabling long-acting drug efficacy. TAK-875 showed potent plasma glucose-lowering action and insulinotropic action during an oral glucose tolerance test in female Wistar fatty rats with impaired glucose tolerance. TAK-875 is currently in clinical trials for the treatment of type 2 diabetes mellitus. |
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| DC75295 |
Tacrolimus anhydrous |
Tacrolimus, also known as FK-506, is an immunosuppressive drug used mainly after allogeneic organ transplant to reduce the activity of the patient's immune system and to lower the risk of organ rejection. It is also used in a topical preparation in the treatment of atopic dermatitis (eczema), severe refractory uveitis after bone marrow transplants, exacerbations of minimal change disease, TH2-mediated diseases such as Kimura's disease, and the skin condition vitiligo. FK-506 is a macrolide isolated from the fungus Streptomyces tsukubaensis. Note: this product is replaced by tacrolimus hydrate (CAT#592996) |
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| DC75296 |
Ozanimod |
Ozanimod, also known as RPC1063, is a selective sphingosine 1 phosphate receptor modulators and methods which may be useful in the treatment of S1P1-associated diseases. Ozanimod has demonstrated efficacy in treating various diseases such as depression, fibromyalgia and obesity. |
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| DC75297 |
T-1095 |
T-1095 is a potent and selective inhibitor of Na+-glucose cotransporters (SGLTs). T-1095 may be a useful antidiabetic drug. Long-term treatment with T-1095 causes sustained improvement in hyperglycemia and prevents diabetic neuropathy in Goto-Kakizaki Rats. Chronic administration of T-1095 (0.1% w w(-1) pellet chow, for 12 weeks) decreased blood glucose and haemoglobin A(1C) levels, and improved glucose intolerance in db/db mice. The age-related decrease in plasma insulin levels was markedly inhibited and there was a 2.5 fold increase of insulin content in the pancreas of T-1095-treated db/db mice. T-1095 improved the metabolic abnormalities and inhibit the development of diabetic complications in db/db mice. |
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| DC75298 |
JNJ-31020028 |
JNJ-31020028 is a selective brain penetrant small molecule antagonist of the neuropeptide Y Y(2) receptor. JNJ-31020028 bound with high affinity (pIC(50) = 8.07 +/- 0.05, human, and pIC(50) = 8.22 +/- 0.06, rat) and was >100-fold selective versus human Y(1), Y(4), and Y(5) receptors. JNJ-31020028 was demonstrated to be an antagonist (pK(B) = 8.04 +/- 0.13) in functional assays. JNJ-31020028 occupied Y(2) receptor binding sites (approximately 90% at 10 mg/kg) after subcutaneous administration in rats. JNJ-31020028 increased norepinephrine release in the hypothalamus, consistent with the colocalization of norepinephrine and neuropeptide Y. In a variety of anxiety models, JNJ-31020028 was found to be ineffective, although it did block stress-induced elevations in plasma corticosterone, without altering basal levels, and normalized food intake in stressed animals without affecting basal food intake. |
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| DC75299 |
LCZ696 |
LCZ696 is a potent ARNi inhibitor and an investigational drug to treat heart failure. Chemically, LCZ696 is a mixture of valsartan and sacubitril in a 1:1 molar ratio. As of 2014 it is being developed by Novartis. LCZ696 is co-crystallized valsartan and sacubitril, in a one-to-one molar ratio. According to Sci-Finder database, LCZ696 has a formula as (valsartan)(sacubitril)(3Sodium)(5/2 hydrate), or (2 valsartan)(2 sacubitril) (6 Sodium)(5 hydrate), which has results C96H120N12Na6O21. Molecular Weight: 1915.99 . However, according to wikipedia, One LCZ696 complex consists of 6 valsartan anions, 6 sacubitril anions, 18 sodium cations, and 15 molecules of water, resulting in the molecular formula C288H330N36Na18O48·15H2O and a molecular mass of 5748.03 g/mol. The substance is a white powder consisting of thin hexagonal plates. It is stable in solid form as well as in aqueous (watery) solution with a pH of 5 to 7, and has a melting point of about 138 °C (280 °F).(http://en.wikipedia.org/wiki/Valsartan/sacubitril) |
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| DC75300 |
ML241 free base |
ML241 is a potent and selective inhibitors of p97 ATPase. ML241 inhibit p97 ATPase with IC(50) values of 100 nM. ML241 inhibits degradation of a p97-dependent but not a p97-independent proteasome substrate in a dual-reporter cell line. ML241 may be a novel agent for the chemotherapy of cancer, and provide a rationale for developing pathway-specific p97 inhibitors. |
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| DC75301 |
Vincristine free base |
Vincristine is a natural alkaloid isolated from the plant Vinca rosea Linn with antimitotic and antineoplastic activities. Vincristine binds irreversibly to microtubules and spindle proteins in S phase of the cell cycle and interferes with the formation of the mitotic spindle, thereby arresting tumor cells in metaphase. This agent also depolymerizes microtubules and may also interfere with amino acid, cyclic AMP, and glutathione metabolism; calmodulin-dependent Ca++ -transport ATPase activity; cellular respiration; and nucleic acid and lipid biosynthesis. Note: Cat#100920A was changed to Cat#100963 |
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| DC75302 |
Sacubitril calcium salt |
Sacubitril, also known as AHU377, is angiotensin receptor neprilysin inhibitor being studied for use in combination with valsartan for heart failure. Sacubitril is a prodrug that is activated to LBQ657 by de-ethylation via esterases. LBQ657 inhibits the enzyme neprilysin, which is responsible for the degradation of atrial and brain natriuretic peptide, two blood pressure lowering peptides that work mainly by reducing blood volume. |
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| DC75303 |
CP-376395 free base |
CP-376395 is a CRF1-selective antagonist. CRF1 receptor signaling regulates food and fluid intake in the drinking-in-the-dark model of binge alcohol consumption |
|
| DC75304 |
Varlitinib |
Varlitinib, also known as ARRY-543 and ASLAN001, is an orally bioavailable inhibitor of the epidermal growth factor receptor family with potential antineoplastic activity. Varlitinib selectively and reversibly binds to both EGFR (ErbB-1) and Her-2/neu (ErbB-2) and prevents their phosphorylation and activation, which may result in inhibition of the associated signal transduction pathways, inhibition of cellular proliferation and cell death. EGFR and Her-2 play important roles in cell proliferation and differentiation and are upregulated in various human tumor cell types. |
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